【药物名称】Diclondazolic acid, Lonidamine, KN-228, AF-1890, Doridamina
化学结构式(Chemical Structure):
参考文献No.47005
标题:Substituted 1-benzyl-1H-indazole-3-carboxylic acids and derivatives thereof
作者:Palazzo, G.; Silvestrini, B. (ACRAF SpA)
来源:DE 2310031; FR 2181773; GB 1381422; US 3895026
合成路线图解说明:

By condensation of 1H-indazole-3-carboxylic acid (I) with 2,4-dichlorobenzyl chloride (II) by means of NaOH in water heated over a steam bath.

合成路线图解说明:

The alkylation of ethyl 1H-indazole-3-carboxylate (I) with 4-chloro-2-methylbenzyl chloride (II) by means of sodium ethoxide in refluxing ethanol gives ethyl 1-(4-chloro-2-methylbenzyl)-1H-indazole-3-carboxylate (III), which is then hydrolyzed with NaOH in refluxing ethanol - water.

参考文献No.49347
标题:Lonidamine
作者:Hillier, K.
来源:Drugs Fut 1979,4(4),265
合成路线图解说明:

By condensation of 1H-indazole-3-carboxylic acid (I) with 2,4-dichlorobenzyl chloride (II) by means of NaOH in water heated over a steam bath.

参考文献No.607170
标题:1-Halobenzyl-1H-3-carboxylic acids. A new class of antispermatogenic agents
作者:Corsi, G.; Palazzo, G.
来源:J Med Chem 1976,19(6),778-783
合成路线图解说明:

By condensation of 1H-indazole-3-carboxylic acid (I) with 2,4-dichlorobenzyl chloride (II) by means of NaOH in water heated over a steam bath.

合成路线图解说明:

The alkylation of ethyl 1H-indazole-3-carboxylate (I) with 4-chloro-2-methylbenzyl chloride (II) by means of sodium ethoxide in refluxing ethanol gives ethyl 1-(4-chloro-2-methylbenzyl)-1H-indazole-3-carboxylate (III), which is then hydrolyzed with NaOH in refluxing ethanol - water.

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